- gamma-lactones alpha,beta- and beta,gamma-fused to carbocycles as novel antiproliferative drugs
[作者:Leon, LG; Machin, RP; Rodriguez, CM; Ravelo, JL; Martin, VS; Padron, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5171-5173 , 文章类型: Article,,卷期:2008年18-19]
- A set of gamma-lactones alpha,beta-fused and beta,gamma-fused to carbocycles have been synthesized and evaluated for their in vitro antiproliferative activities using the human cancer cell lines SW1573 (lung), T-47D (bre...
- Synthesis and antiproliferative activity of unnatural enantiomers of 7-epi-goniofufurone and crassalactone C
[作者:Popsavin, V; Benedekovic, G; Sreco, B; Popsavin, M; Francuz, J; Kojic, V; Bogdanovic, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5178-5181 , 文章类型: Article,,卷期:2008年18-19]
- A facile synthesis of 7-epi-(-)-goniofufurone as well as the first synthesis of (-)-crassalactone C was achieved starting from D-xylose. A comparison of their in vitro antitumour activities with those observed for the co...
- Design, synthesis and antiproliferative activity of two new heteroannelated (-)-muricatacin mimics
[作者:Popsavin, V; Sreco, B; Benedekovic, G; Popsavin, M; Francuz, J; Kojic, V; Bogdanovic, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5182-5185 , 文章类型: Article,,卷期:2008年18-19]
- Two new (-)-muricatacin mimics bearing a furano-furanone ring and an oxygen isostere in the side chain have been designed and synthesized and their in vitro antiproliferative activity was evaluated against several human ...
- Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors
[作者:Hanan, EJ; Fucini, RV; Romanowski, MJ; Elling, RA; Lew, W; Purkey, HE; VanderPorten, EC; Yang, WJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5186-5189 , 文章类型: Article,,卷期:2008年18-19]
- A series of 2-amino-isoxazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors. Key SAR and crystallographic data are discussed. More advanced analogues inhibit Plk1 with good enzymatic activity...
- New functionalized 1,2,4-trioxepanes: Synthesis and antimalarial activity against multi-drug resistant P. yoelii in mice
[作者:Singh, C; Pandey, S; Kushwaha, AK; Puri, SK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5190-5193 , 文章类型: Article,,卷期:2008年18-19]
- A series of new amino functionalized 1,2,4-trioxepanes8-16 and ester functionalized 1,2,4-trioxepanes 17-19 have been synthesized and evaluated against multi-drug resistant Plasmodium yoelii in Swiss mice. Amino function...
- Synthesis of nuclease-resistant siRNAs possessing benzene-phosphate backbones in their 3 '-overhang regions
[作者:Ueno, Y; Inoue, T; Yoshida, M; Yoshikawa, K; Shibata, A; Kitamura, Y; Kitade, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5194-5196 , 文章类型: Article,,卷期:2008年18-19]
- We describe the synthesis and silencing activities of siRNA possessing N-1-[3,5-bis(hydroxymethyl) phenyl] thymine (b(t)) in their 3'-overhang regions. We found that an siRNA possessing b(t) in the 3'-overhang region was...
- Design, synthesis and characterization of podocarpate derivatives as openers of BK channels
[作者:Cui, YM; Yasutomi, E; Otani, Y; Yoshinaga, T; Ido, K; Sawada, K; Ohwada, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5197-5200 , 文章类型: Article,,卷期:2008年18-19]
- We found that the podocarpic acid structure provides a new scaffold for chemical modulators of large-conductance calcium-activated K+ channels (BK channels). Structure-activity analysis indicates the importance of both t...
- Novel BK channel openers containing dehydroabietic acid skeleton: Structure-activity relationship for peripheral substituents on ring C
[作者:Cui, YM; Yasutomi, E; Otani, Y; Yoshinaga, T; Ido, K; Sawada, K; Ohwada, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5201-5205 , 文章类型: Article,,卷期:2008年18-19]
- A series of dehydroabietic acid (DHAA, 2) derivatives was synthesized and evaluated as BK channel openers in an assay system of CHO-K1 cells expressing hBK alpha channels. Systematic modi. cations of the peripheral funct...
- Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: Chemistry, biological activities, and molecular modeling
[作者:Tong, YS; Stewart, KD; Thomas, S; Przytulinska, M; Johnson, EF; Klinghofer, V; Leverson, J; McCall, O; Soni, NB; Luo, Y; Lin, NH; Sowin, TJ; Giranda, VL; Penning, TD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5206-5208 , 文章类型: Article,,卷期:2008年18-19]
- A series of isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones were synthesized as potent inhibitors against Pim-1 and Pim-2 kinases. The structure-activity-relationship studies started from a high-throughput screening hit and ...
- Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha 4 beta 2 nicotinic acetylcholine receptor potentiators
[作者:Albrecht, BK; Berry, V; Boezio, AA; Cao, L; Clarkin, K; Guo, WH; Harmange, JC; Hierl, M; Huang, LY; Janosky, B; Knop, J; Malmberg, A; McDermott, JS; Nguyen, HQ; Springer, SK; Waldon, D; Woodin, K; McDonough, SI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5209-5212 , 文章类型: Article,,卷期:2008年18-19]
- The discovery of a series of small molecule alpha 4 beta 2 nAChR potentiators is reported. The structure-activity relationship leads to potent compounds selective against nAChRs including alpha 3 beta 2 and alpha 3 beta ...
- Tacrine based human cholinesterase inhibitors: Synthesis of peptidic-tethered derivatives and their effect on potency and selectivity
[作者:Butini, S; Guarino, E; Campiani, G; Brindisi, M; Coccone, SS; Fiorini, I; Novellino, E; Belinskaya, T; Saxena, A; Gemma, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5213-5216 , 文章类型: Article,,卷期:2008年18-19]
- Tacrine based reversible inhibitors of cholinesterases (ChEIs) containing peptidic tethers were synthesized to interact with specific regions at the gorge level, and their potency was determined with human ( h) acetylcho...
- Design and synthesis of 3-pyrazolyl-thiophene, thieno[2,3-d]pyrimidines as new bioactive and pharmacological activities
[作者:Hafez, HN; El-Gazzar, ABA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5222-5227 , 文章类型: Article,,卷期:2008年18-19]
- Two series of 5-ethyl-2-amino-3-pyrazolyl-4- methylthiophenecarboxylate and 2-thioxo-N-3-aminothieno[ 2,3-d]pyrimidines were prepared from 3,5-diethyl-2-amino-4-methylthio-phenecaboxylate and evaluated as anti-inflammato...
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